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At least 523 records · Page 29Linked to original sources
PubMed2000

Flavone-8-acetic acid (Flavonoid) profoundly reduces platelet-dependent thrombosis and vasoconstriction after deep arterial injury In vivo.

BACKGROUND: Flavone-8-acetic acid (FAA; [Flavonoid]), an adjuvant antitumor drug, inhibits ristocetin-induced aggregation of human platelets. The effect of FAA on platelet-dependent thrombosis was studied in vivo in the porcine carotid artery after deep arterial injury by balloon angioplasty. METHODS AND RESULTS: (111)In-labeled autologous platelet and (125)I-labeled porcine fibrin(ogen) deposition, and the incidence of macroscopic mural thrombosis onto deeply injured artery (tunica media) were compared in 20 pigs (40+/-1 kg [mean+/-SEM], body surface area=1.0+/-0.1 m(2)), randomized to FAA bolus (n=10) of 5.5g/m(2), followed by an infusion at 0.14g. m(-2). min(-1) or placebo (n=10). Vasoconstriction was measured immediately beyond the dilated segment using quantitative angiography. Platelet deposition (x10(6)/cm(2) of carotid artery) was reduced over 12-fold in pigs treated with FAA (13+/-3 versus 164+/-51, P=0.001) compared with placebo. Fibrin(ogen) deposition (x10(12) molecules/cm(2) of carotid artery) did not significantly differ in FAA-treated pigs versus placebo (40+/-8 versus 140+/-69, P=0.08). Large mural thrombi were present in 100% of placebo-treated pigs versus very small thrombi in 40% of FAA-treated pigs (P=0.005). Vasoconstriction was reduced from 46+/-6% in the placebo group to 15+/-3% in the FAA group (P<0.001). Plasma level of FAA before angioplasty was 515+/-23 microgram/mL. The activated partial thromboplastin time was unchanged. The bleeding time was >2SD above the normal mean in 4 of 5 treated pigs (increased from 157+/-29 to 522+/-123 s). CONCLUSIONS: FAA markedly reduced platelet deposition, mural thrombi, and injury-induced vasoconstriction after deep arterial injury, suggesting that a major inhibition of platelet glycoprotein Ibalpha may be beneficial therapy.

Animals↗
PubMed1999

In-vivo and in-vitro assessment of the free-radical-scavenger activity of Ginkgo flavone glycosides at high concentration.

Free radicals are involved in numerous skin diseases, especially inflammatory reactions and photosenescence. To identify possible free-radical scavenging by an original terpene-free Ginkgo biloba extract containing 33% Ginkgo flavone glycosides, mostly quercetin and kaempferol derivatives, we studied its activity by means of in-vitro and in-vivo experiments, using superoxide dismutase (SOD) as a positive control. By means of an in-vitro electron-spin resonance (ESR) assay we compared the activity of the Ginkgo extract with that of its two aglycones, quercetin and kaempferol. Quercetin and Ginkgo extract had significant antioxidant properties without pro-oxidant effect. In contrast, kaempferol, above an optimum antioxidant concentration, behaved as a pro-oxidant. The in-vivo experiments were conducted on an anti-inflammatory model. The cutaneous blood flux which reflects the skin inflammatory level was recorded by means of a laser Doppler perfusion imager. The data confirmed the free-radical-scavenging property of both Ginkgo extract and SOD. The Ginkgo extract significantly inhibited (37%) cutaneous blood flux to the same extent as SOD. These data confirmed the antioxidant property of Ginkgo extract. A complementary spin-trapping technique would enable identification of the free radicals involved. This Ginkgo extract should be useful for protection of the skin against free radicals.

Antioxidants↗
PubMed2006

Pharmacokinetics of 7-carboxymethyloxy-3',4',5-trimethoxy flavone (DA-6034), a derivative of flavonoid, in mouse and rat models of chemically-induced inflammatory bowel disease.

The pharmacokinetics (including distribution in the gastrointestinal tract) of 7-carboxymethyloxy-3',4',5-trimethoxy flavone (DA-6034) has been investigated in several mouse and rat models of chemically-induced inflammatory bowel disease (IBD). In the female ICR mouse model, IBD was induced by dextran sulfate and the mice administered 30 mg kg(-1) DA-6034 intravenously or orally. In the male SJL mouse model of IBD induced by oxazolone, 30 mg kg(-1) DA-6034 was administered orally. In the male Sprague-Dawley rat model of IBD induced by trinitrobenzene sulfonic acid (TNBS), 10 mg kg(-1) DA-6034 was administered intravenously and orally. After intravenous administration, the total area under the plasma concentration-time curve from time zero to the last measured time, t, in plasma (AUC(0-t)) values were comparable between control and dextran sulfate-induced IBD mice, and between control and TNBS-induced rats. This suggested that the disposition of DA-6034 was not affected considerably by dextran sulfate in mice and TNBS in rats. However, after oral administration in mice and rats with IBD, the AUC(0-t) values were greater compared with the respective controls. This could have been due to an increase (slow) in the gastrointestinal transit time (in IBD mice and rats, the percentages of the oral dose recovered from the rinsing fluid of the small intestine and large intestine as unchanged drug were greater and smaller, respectively), and an increase in intestinal permeability.

Administration, Oral↗
PubMed2003

Flavone C-glycosides from Viola yedoensis MAKINO.

A new flavone C-glycoside, apigenin 6-C-alpha-L-arabinopyranosyl-8-C-beta-L-arabinopyranoside, has been isolated from Viola yedoensis together with the known compounds, apigenin 6,8-di-C-alpha-L-arabinopyranoside, apigenin 6-C-alpha-L-arabinopyranosyl-8-C-beta-D-glucopyranoside (isoschaftoside), apigenin 6-C-beta-D-glucopyranosyl-8-C-alpha-L-arabinopyranoside (schaftoside), apigenin 6-C-beta-D-glucopyranosyl-8-C-beta-L-arabinopyranoside (neoschaftoside), apigenin 6,8-di-C-beta-D-glucopyranoside (vicenin-2), apigenin 6-C-alpha-L-arabinopyranosyl-8-C-beta-D-xylopyranoside, apigenin 6-C-beta-D-xylopyranosyl-8-C-alpha-L-arabinopyranoside, luteolin 6-C-beta-D-glucopyranoside (isoorientin) and luteolin 6-C-alpha-L-arabinopyranosyl-8-C-beta-D-glucopyranoside (isocarlinoside). The structures were determined by spectroscopic methods and new or revised (1)H- and (13)C-NMR spectral assignments are proposed for some compounds.

Flavonoids↗
PubMed2003

A new chalcone and a flavone from Andrographis neesiana.

Two new flavonoids, 2',4',6',2,3,4-hexamethoxychalcone (1) and 5-hydroxy-7,2',5'-trimethoxyflavone (2) together with a known flavone glycoside, echioidinin 5-O-beta-D-glucopyranoside (3) were isolated from the whole plant of Andrographis neesiana, and the structures were elucidated by electrospray ionization tandem mass spectrometry (ESI-MS/MS) and one- and two-dimensional (1D- and 2D)-NMR spectral studies including 1H-1H correlation spectroscopy (COSY), heteronuclear single quantum coherence (HSQC), heteronuclear multiple bond connectivity (HMBC) and nuclear Overhauser enhancement spectroscopy (NOESY) experiments.

Andrographis↗
PubMedDate not supplied

A new oxyprenyl coumarin and highly methylated flavones from the exudate of Ozothamnus lycopodioides (Asteraceae).

A new oxyprenyl coumarin was isolated from the lipophilic exudate of Ozothamnus lycopodioides. Its structure was established as 7-(3,3'-dimethylallyloxy)-5-hydroxy-6-methoxycoumarin from its UV, MS and NMR spectral data, especially two dimensional experiments. In addition to six earlier reported flavonols, we found four highly substituted flavones, including two rare methylenedioxyflavones.

Asteraceae↗
PubMedDate not supplied

The unique occurrence of the flavone aglycone tricetin in Myrtaceae pollen.

In pollen, flavonoids are usually found as glycosides and in particular, flavonol 3-O-diglycosides. However, in members of the Myrtaceae, subfamily Leptospermoideae, the rare flavone aglycone tricetin, along with other flavonoid aglycones including 3-O-methyl quercetin and luteolin, have been found to comprise a significant portion of the constituent flavonoids.

Animals↗
PubMedDate not supplied

A new highly oxygenated flavone from Veronia saligna.

A new highly oxygenated flavone, namely 8,3'-dihydroxy-5,6,7,4'-tetramethoxyflavone (1), together with other five known flavonoids were isolated from the tropical plant Vernonia saligna. Their structures were established on the basis of spectral (MS, IR, UV, 1D & 2D NMR) measurement and chemical evidence.

China↗
PubMed2004

Structural analysis of selected characteristic flavones by electrospray tandem mass spectrometry.

Seven structure analogical flavonoid aglycones have been analyzed using electrospray ionization tandem mass spectrometry (ESI-MSn) in the negative-ion mode. The spectra obtained ESI-MSn allowed us to propose plausible schemes for their fragmentation mechanism. By analyzing the product ions spectra of deprotonated molecule ions [M-H](-), some neutral diagnostic losses and specific retro Diels-Alder fragments were obtained. By using all of these characteristic fragment ions we can specially differentiate the flavone isomer.

Flavonoids↗
PubMedDate not supplied

Combined treatments of heat, radiation, or cytokines with flavone acetic acid on the growth of cultured endothelial cells.

The antitumour effects of flavone acetic acid (FAA) against a broad spectrum of established experimental tumours has been demonstrated. Damage to the vasculature, which rapidly disrupts blood flow and induces haemorrhagic necrosis, is believed to be a major mechanism contributing to the observed antitumour effects. Despite these established observations, FAA has shown little effect against human tumours. However, other applications of FAA, for examples, for an extended period of treatments or in combination with other antitumour modalities, have not been sufficiently explored. In order to test the direct effects of FAA on vasculature, endothelial cells isolated from human umbilical vein (HUVEC) and bovine pulmonary artery (CPAEC) were used in this study. FAA at the concentrations of 50 to 200 micrograms/ml causes reduction in cell number (from 20 to > 30% of the cells) of HUVEC as measured by MTT assay after 1, 3, and 5 h of treatment at 37 degrees C. FAA did not produce significant effects on similarly treated human squamous cell carcinoma, cell line UM-SCC-2. After 1 h treatment of FAA at 300 micrograms/ml, a large number of HUVECs failed to react with an actin stain, NBD-phallacidin. The growth of HUVECs and CPAEC in the presence of FAA for 1-3 days was progressively reduced. The number of HUVEC treated for 3 days at the concentrations of 100, 200, and 300 micrograms/ml were reduced by 75-86% in comparison with the control culture. The experiments with CPAEC showed similar results. The inhibition of the growth of endothelial cells by FAA was enhanced when it combines with tumour necrosis factor-alpha but not with interleukin-1, interferon-gamma, heat, or radiation. We observed that FAA can initiate both immediate effects and growth inhibition on cultured endothelial cells. These results support the notion that FAA rapidly induces vasculature damage. Furthermore, cytokines such as tumour necrosis factor-alpha can enhance the toxicity of FAA on endothelial cells.

Animals↗
PubMedDate not supplied

The in vivo interaction between flavone acetic acid and hyperthermia.

The in vivo interaction between flavone acetic acid (FAA) and hyperthermia was studied in a C3H mammary carcinoma grown in the feet of female CDF1 mice and in normal foot skin. FAA was intraperitoneally injected prior to local tissue heating in restrained non-anaesthetized animals. Alone, FAA at doses of 100 mg/kg and above, inhibited tumour growth in a dose-dependent fashion. FAA also enhanced the tumour response to heat, the effect being dependent on both the time interval between the two modalities and the FAA dose, the greatest effect occurring when FAA doses of > or = 150 mg/kg preceeded heat by 3-48 h. These effects of FAA correlated with the drug's ability to decrease tumour blood perfusion measured using the RbCl extraction procedure. Injecting 150 mg/kg FAA 3 h before heating (42.7 degrees C) resulted in a 2.2-fold increase in tumour heat damage, but had little effect on the response of normal foot skin in non-tumour-bearing mice. However, this treatment gave a 2.0-fold increase in normal tissue damage when the skin experiments were repeated in tumour-bearing animals. These effects in skin occurred in the absence of any blood perfusion changes, but appeared to be associated with FAA-induced TNF-alpha production.

Animals↗
PubMed2004

Effects of Radix Puerariae flavones on liver lipid metabolism in ovariectomized rats.

AIM: To study the effects of Radix Puerariae flavones (RPF) on liver lipid metabolism in ovariectomized (OVX) rats. METHODS: Forty adult female Wistar rats were randomly divided into four groups: OVX group; sham-OVX group; OVX+estrogen group and OVX+RPF group. One week after operation rats of the first two groups were treated with physiological saline, rats of OVX+estrogen group with estrogen (1 mg/kg.b.w.) and rats of OVX+RPF group with RPF (100 mg/kg.b.w.), respectively for 5 weeks. After the rats were killed, their body weight, the weight of the abdominal fat and uterus were measured, and the levels of total cholesterol (TC) and triglyceride (TG) in liver homogenate were determined. RESULTS: Compared with the sham-OVX group, the body mass of the rats in OVX group was found increased significantly; more abdominal fat in store; TC and TG in liver increased and uterine became further atrophy. As a result, the RPF was found to have an inhibitive action on those changes of various degrees. CONCLUSION: RPF has estrogen-like effect on lipid metabolism in liver and adipose tissue.

Abdomen↗
PubMedDate not supplied

Oxidative stress contributes to the anti-proliferative effects of flavone acetic acid on endothelial cells.

The synthetic flavonoid flavone acetic acid (FAA) has anti-tumor activity against a variety of transplanted tumors in mice through mechanisms which likely involve effects on tumor vasculature and the host immune system. The aims of the present in vitro study were to compare the sensitivity of tumor and endothelial cells to FAA treatment and to assess if nitric oxide and superoxide are involved in the FAA-mediated suppression of cell proliferation. FAA at 1 mM concentration was approximately two times more effective in suppressing proliferation of endothelial than tumor cells. The anti-proliferative effect of 1 mM FAA on endothelial cells was partially blocked by inhibitors to various superoxide-producing enzymes (xanthine oxidase, cyclooxygenase, poly-ADP-ribose polymerase, ribonucleotide reductase) and completely inhibited by the direct scavengers of superoxide lucigenin and Tiron. In contrast, inhibitors of nitric oxide were unable to prevent the effects of FAA on proliferation. FAA induced apoptosis of endothelial cells, which was not affected by inhibitors of nitric oxide or superoxide. Our data imply that FAA inhibits proliferation of endothelial cells by a superoxide-dependent mechanism and induces apoptosis by a nitric oxide and superoxide-independent mechanism.

Animals↗
PubMed2000

Antidiabetic effect of Oenanthe javanica flavone.

AIM: To study the antidiabetic effect of Oenanthe javanica flavone (OjF). METHODS: Mice were injected i.v. with alloxan 90 mg.kg-1 to induce diabetes. Blood glucose, serum lipid, and pancreatic amylase were determined with Automatic Biochemistry Analysor. Serum insulin was determined by radioimmunoassay. The pancreas and islets were examined under microscope. RESULTS: OjF 200 mg.kg-1 reduced the blood glucose in normal mice from 0.5 to 6 h after a single administration ig. OjF 200 and 400 mg.kg-1 ig daily for 10 d decreased the blood glucose in alloxan-induced hyperglycemic mice (P < 0.05, P < 0.01). OjF promoted the release of insulin both in normal and in diabetic mice. OjF decreased serum triglyceride and raised the lowered pancreatic amylases in diabetic mice (P < 0.01, P < 0.01). The islet-injured changes of OjF-treated group were similar to those of control in histology examination, but to a lesser degree. CONCLUSION: OjF possessed the hypoglycemic and hypotriglyceride actions, mainly concerned with promoting release of insulin from B-cells in islets of langerhans.

Amylases↗
PubMed2000

Role of ATP sensitive potassium channel on 7-hydroxy flavone induced antinociception and possible association with changes in glycaemic status.

Opioid type of analgesics open ATP sensitive potassium channel at the cellular level to produce antinociceptive response. These channels have also been shown to modulate insulin secretion by the pancreas. 7-hydroxy flavone, an antinociceptive agent shown to act through opioid pathways was investigated for its effect on glycaemic state and associated algesic state. The involvement of ATP sensitive potassium channel in the action was examined by using glybenclamide. The result reveal that 7-HF per se did not elicit any significant change in the glycaemic state simultaneously eliciting antinociceptive response as tested by acetic acid induced abdominal constriction assay procedure. Glibenclamide treatment attenuated the antinociceptive effect of 7-HF and while maintained its hypoglycaemic response. The present finding suggest that 7-HF induces antinociception like morphine, utilise ATP sensitive potassium channel at the cellular level and do not suggest a cause-effect relationship between the changes in the glycaemic and algesic state. Possibly, insulin which is controlled by ATP sensitive potassium channel at the cellular level might also modulate antinociception exhibiting a cause-effect relationship between them.

Adenosine Triphosphate↗
PubMed1975

Action in human blood of methoxylated flavones which confer disease resistance on both plants and animals: concept of a dietary conditioned mechanism of defense against disease-1,2.

The antiadhesive action of methoxylated flavones on cells in blood of hospitalized patients was significantly associated with calcium, probably at membrane interfaces. This action is consistent with the role of calcium in cell aggregation and disaggregation. These and other recent findings suggest the body has a capacity for an environmentally related dietary conditioned, resistance to disease. The concept is based on evidence that phenylbenzo-gamma-pyrone derivatives, methyoxylated flavonoids and related compounds, synthesized in plants with antiviral, antifungal and bacteriostatic action may be absorbed into the body and attach reversibly to blood cells. In the body, in addition to any potential action against pathogens, certain of these compounds potentiate enzymes which detoxify carcinogenic hydrocarbons, exhibit antiinflammatory activity, exert antiadhesive action on blood cells and show antithrombogenic activity. The evidence indicates that of this class of compounds, a few are broad spectrum in their action, while several others possess one or another of the above functions. Also, some compounds are active in practically all subjects while others are active only in some patients. Specificities appear to be involved in action of the compounds on both pathogens and body processes.

Alkaline Phosphatase↗
PubMed1975

Spectrophotometric estimation of individual flavone glycosides in three Euphorbia species.

Two spectrophotometric methods (conventional and differential) are carried out for the estimation of flavone glycosides (hyperoside and/or kaempferol-3-beta-glucoside) in Euphorbia paralias L., and Euphorbia helioscopia L. The glycosides are extracted with methanol from the aerial parts of the different Euphorbia species, separated on silica gel chromatoplates, and eluted by refluxing with methanol (80%). The absorbance value (conventional method) and the delta absorbance value (differential method) of the prepared glycosidal solutions are measured. The results of both methods are of conveinent reproducibility.

Chromatography, Thin Layer↗